GLP-1 Receptors

Cat. No.

A26148

CAS No.

439087-68-0

(S)-Elobixibat

Synonyms: (S)-A 3309; (S)-AZD 7806

(S)-Elobixibat is a selective inhibitor of the intestinal bile acid transporter (IBAT). It effectively lowers LDL cholesterol levels, enhances serum levels of GLP-1, and promotes colonic motility, making it a valuable tool in metabolic syndrome research. This compound is utilized in studies related to constipation, dyslipidemia, non-alcoholic fatty liver disease, and liver tumors.

Cat. No.

A43474

CAS No.

330204-04-1

AGFAGDDAPR

AGFAGDDAPR is a competitive and orally active inhibitor of dipeptidyl peptidase-IV (DPP-IV). By inhibiting DPP-IV, AGFAGDDAPR increases levels of glucagon-like peptide-1 (GLP-1), which stimulates insulin secretion, enhances β-cell function, and suppresses excessive α-cell proliferation, resulting in beneficial anti-diabetic effects. This peptide is suitable for investigating mechanisms and therapeutic approaches related to type 2 diabetes.

Cat. No.

A43478

CAS No.

440100-64-1

K579

K579 is a potent dipeptidyl peptidase IV (DPPIV) inhibitor that exhibits oral bioactivity. This compound effectively mitigates blood glucose elevation by increasing plasma insulin levels and enhancing the active forms of glucagon-like peptide-1 (GLP-1). K579 is suitable for research applications focused on diabetes and glucose metabolism regulation.

Cat. No.

A43515

CAS No.

486460-31-5

DPP-4-IN-18

Synonyms: Sitagliptin impurity 3

DPP-4-IN-18 is a potent and selective Dipeptidyl Peptidase-4 (DPP-4) inhibitor with an IC50 of 27 nM. By inhibiting DPP-4, this compound prevents the degradation of glucagon-like peptide 1 (GLP-1), leading to increased levels of active GLP-1. DPP-4-IN-18 is primarily utilized in research focused on type 2 diabetes and related metabolic disorders.

Cat. No.

A43536

CAS No.

1123219-12-4

DPP-4-IN-10

DPP-4-IN-10 is a potent DPP-4 inhibitor that acts to prevent the degradation of glucagon-like peptide-1 (GLP-1) and gastric inhibitory polypeptide (GIP). By inhibiting DPP-4, this compound may enhance glycemic control in individuals with type 2 diabetes mellitus (T2DM). Its oral bioavailability makes it suitable for pharmacological studies focused on glucose metabolism and diabetes management.

Cat. No.

A43538

CAS No.

651055-26-4

ASP8497

ASP8497 is a competitive inhibitor of dipeptidyl peptidase IV (DPP-IV), which plays a critical role in glucose metabolism. This compound effectively reduces blood glucose levels and elevates plasma active GLP-1 and insulin concentrations without inducing hypoglycemia in fasted normal mice. ASP8497 is suitable for research applications focused on antihyperglycemic mechanisms and glucose regulation.

Cat. No.

A43553

CAS No.

141979-19-3

16-Hydroxycleroda-3,13-dien-15,16-olide

Synonyms: 16ξ-Hydroxycleroda-3,13-dien-15,16-olide

16-Hydroxycleroda-3,13-dien-15,16-olide is a potent dipeptidyl peptidase 4 (DPP-4) inhibitor, targeting the serine protease class of enzymes. This clerodane diterpene demonstrates key biological activities, including the down-regulation of lipopolysaccharide (LPS)-induced ERK phosphorylation in myocytes and inhibition of glucagon-like peptide-1 (GLP-1) induced protein kinase A (PKA) expression. Additionally, it exhibits hypolipidemic, hepatoprotective, and hypoglycemic effects, making it a valuable compound for research in metabolic and cardiovascular diseases.

Cat. No.

A43576

CAS No.

667865-69-2

TS-021

TS-021 is a selective, orally active, reversible DPP-IV inhibitor with long-lasting effects. It demonstrates significant selectivity against DPP-8 and DPP-9, exceeding 600-fold and 1,200-fold, respectively, as well as a greater than 15,000-fold selectivity over other peptidases. With an IC50 value of 5.34 nM for DPP-IV inhibition in human plasma, TS-021 is effective in enhancing active GLP-1 levels and exhibits potent antihyperglycemic activity, making it valuable for research in diabetes and metabolic disorders.

Cat. No.

A60608

CAS No.

2089617-83-2

MS012

MS012 is a selective glucagon-like peptide (GLP) inhibitor with an IC50 value of 7 nM. This compound serves as a valuable tool in the investigation of GLP dysregulation associated with various conditions, including cancer, inflammatory diseases, and neuroregenerative disorders. Its application in research may facilitate the understanding of GLP's role in these pathophysiological processes.

Cat. No.

A60630

CAS No.

3059497-30-9

GIPR antagonist 1

GIPR Antagonist 1 is a potent inhibitor of the glucose-dependent insulinotropic polypeptide receptor (GIPR) with an IC50 of 4.8 nM. By effectively blocking GIPR signaling, this compound serves as a valuable tool in the study of type 2 diabetes and obesity. Its ability to modulate GIPR activity makes it significant for research focused on glucose metabolism and insulin regulation.

Cat. No.

A65892

CAS No.

1633824-78-8

Elobixibat hydrate

Synonyms: A 3309 hydrate; AZD 7806 hydrate

Elobixibat hydrate is an orally active inhibitor of the intestinal bile acid transporter (IBAT), demonstrating potent activity with IC50 values of 0.53 nM for human IBAT, 0.13 nM for mouse IBAT, and 5.8 nM for canine IBAT. This compound has been shown to effectively lower LDL cholesterol levels, enhance serum GLP-1 concentrations, and promote colonic motility. Elobixibat hydrate is valuable for research applications related to chronic idiopathic constipation (CIC), dyslipidemia, non-alcoholic fatty liver disease, and the study of liver tumors, particularly in elderly populations.